1024085-01-5

Upstream product

• 126473-61-8 (2E)-1-(4-bromophenyl)-3-(4-fluorophenyl)prop-2-en-1-one 
• 99-90-1 para-bromoacetophenone 
• 459-57-4 4-fluorobenzaldehyde 
• 98991-32-3 1-(4-bromophenyl)-3-(4-fluorophenyl)prop-2-en-1-one 

Downstream Products

• 1365656-14-9 1-N-(3-bromobenzoyl)-3-(4-bromophenyl)-5-(4-fluorophenyl)-4,5-dihydro-1H-pyrazole 
• 1365656-13-8 1-N-(2-fluorobenzoyl)-3-(4-bromophenyl)-5-(4-fluorophenyl)-4,5-dihydro-1H-pyrazole 
• 1403750-47-9 (3-(4-bromophenyl)-5-(4-fluorophenyl)-4,5-dihydro-1H-pyrazol-1-yl)(2,3-dihydrobenzo[b][1,4]dioxin-2-yl)methanone 

Relevant academic research and scientific papers

Preparation, Antiepileptic Activity, and Cardiovascular Safety of Dihydropyrazoles as Brain-Penetrant T-Type Calcium Channel Blockers

A series of dihydropyrazole derivatives was developed as potent, selective, and brain-penetrating T-type calcium channel blockers. An optimized derivative, compound 6c, was advanced to in vivo studies, where it demonstrated efficacy in the WAG/Rij rat model of generalized nonconvulsive, absence-like epilepsy. Compound 6c was not efficacious in the basolateral amygdala kindling rat model of temporal lobe epilepsy, and it led to prolongation of the PR interval in ECG recordings in rodents.

Design, modification and 3D QSAR studies of novel 2,3-dihydrobenzo[b][1,4] dioxin-containing 4,5-dihydro-1H-pyrazole derivatives as inhibitors of B-Raf kinase

Two series of novel 2,3-dihydrobenzo[b][1,4]dioxin-containing 4,5-dihydro-1H-pyrazole derivatives C1-C15 and D1-D15 have been synthesized and evaluated for their B-Raf inhibitory and anti-proliferation activities. Compound C14 ((3-(4-bromophenyl)-5-(2-fluorophenyl)-4,5-dihydro-1H-pyrazol-1-yl)(2,3- dihydrobenzo[b][1,4]dioxin-6-yl)methanone) showed the most potent biological activity against B-RafV600E (IC50 = 0.11 μM) and WM266.4 human melanoma cell line (GI50 = 0.58 μM), being comparable with the positive control Erlotinib and more potent than our previous best compound, while D10 ((2,3-dihydrobenzo[b][1,4]dioxin-2-yl)(5-(3- fluorophenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)methanone) performed the best in the D series (IC50 = 1.70 μM; GI50 = 1.45 μM). The docking simulation was performed to analyze the probable binding models and poses and the QSAR model was built for reasonable design of B-Raf inhibitors in future. The introduction of 2,3-dihydrobenzo[b][1,4]dioxin structure reinforced the combination of our compounds and the receptor, resulting in progress of bioactivity.

Synthesis and anti-inflammatory activity of some 3, 5-diaryl-2-pyrazoline derivatives

Eleven new 3-(4-bromophenyl)-5-(4-flirorophenyl)-2-pyrazoline derivatives 4-9 and 11-15 were synthesized by using 1-(4-bromophenyl)-3-(4-fluorophenyl) prop-2-en-1-one (3). The newly synthesized compounds were evaluated for anti-inflammatory activity against carrageenan edema in albino rats at a dose of 10 mg/kg. All the compounds of this series showed promising anti-inflammatory activity. The most active compound of this series, 7 was found to be most potent, which has shown higher percentage of inhibition of edema than the standard drug indomethacin.